Download or read book The Design Synthesis and Biological Evaluation of Five Two point Diversity scaffolded Libraries written by Crystal Leigh Olson and published by . This book was released on 2006 with total page 294 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Privileged Scaffolds in Medicinal Chemistry written by Stefan Bräse and published by Royal Society of Chemistry. This book was released on 2015-11-20 with total page 486 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.
Download or read book Bioactive Heterocycles written by K. L. Ameta and published by Nova Science Publishers. This book was released on 2013 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a critical and lucid account of various synthetic methodologies and biological activities of different sized bioactive heterocyclic compounds. In effect, this book imparts a great deal of comprehensive reviews about the chemistry and biology of selected groups of heterocycles and natural products including important pharmaceuticals as well as agrochemical pesticides in one handy project. Besides, this compendious effort encompasses different methods of synthesis and biological evaluation of heterocyclic compounds. The main purpose of this book is to share the recent advances and scope of Bioactive Heterocycles for the future avenues in the field. It has specifically been designed by keeping in mind the wide interests of individuals engaged in the design and synthesis of biologically active heterocyclic compounds as well as research scientists in academia and industry. The authors expect this book to be a standard reference in Universities and industrial libraries.
Download or read book Exploiting Chemical Diversity for Drug Discovery written by Paul A Bartlett and published by Royal Society of Chemistry. This book was released on 2007-10-31 with total page 445 pages. Available in PDF, EPUB and Kindle. Book excerpt: Conceptual and technological advances in chemistry and biology have transformed the drug discovery process. Evolutionary pressure among the diverse scientific and engineering disciplines that contribute to the identification of biologically active compounds has resulted in synergistic improvements at every step in the process. Exploiting Chemical Diversity for Drug Discovery encompasses the many components of this transformation and presents the current state-of-the-art of this critical endeavour. From the theoretical and operational considerations in generating a collection of compounds to screen, to the design and implementation of high-capacity and high-quality assays that provide the most useful biological information, this book provides a comprehensive overview of modern approaches to lead identification. Beginning with an introductory overview, subsequent chapters address topics that include the design of chemical libraries and methods for optimizing their diversity; automated and accelerated chemistry; high throughput assay design and detection techniques; and strategies for data analysis and property optimization. Written by experts in the field, both academic and industrial, and illustrated in full colour, this book provides an excellent overview for current practitioners and will also serve as a stimulating resource for future generations. Researchers in organic and medicinal chemistry, the biological and pharmacological sciences, as well as those interested in allied computational and engineering disciplines will value the comprehensive and up-to-date coverage.
Download or read book Epigenetic Drug Discovery written by Wolfgang Sippl and published by John Wiley & Sons. This book was released on 2019-03-25 with total page 504 pages. Available in PDF, EPUB and Kindle. Book excerpt: This broad view of epigenetic approaches in drug discovery combines methods and strategies with individual targets, including new and largely unexplored ones such as sirtuins and methyl-lysine reader proteins. Presented in three parts - Introduction to Epigenetics, General Aspects and Methodologies, and Epigenetic Target Classes - it covers everything any drug researcher would need in order to know about targeting epigenetic mechanisms of disease. Epigenetic Drug Discovery is an important resource for medicinal chemists, pharmaceutical researchers, biochemists, molecular biologists, and molecular geneticists.
Download or read book Coumarin and Its Derivatives written by Maria João Matos and published by Mdpi AG. This book was released on 2021-12-29 with total page 416 pages. Available in PDF, EPUB and Kindle. Book excerpt: Coumarins are widely distributed in nature and can be found in a large number of naturally occurring and synthetic bioactive molecules. The unique and versatile oxygen-containing heterocyclic structure makes them a privileged scaffold in Medicinal Chemistry. Many coumarin derivatives have been extracted from natural sources, designed, synthetized, and evaluated on different pharmacological targets. In addition, coumarin-based ion receptors, fluorescent probes, and biological stains are growing quickly and have extensive applications to monitor timely enzyme activity, complex biological events, as well as accurate pharmacological and pharmacokinetic properties in living cells. The extraction, synthesis, and biological evaluation of coumarins have become extremely attractive and rapidly developing topics. A large number of research and review papers have compiled information on this important family of compounds in 2020. Research articles, reviews, communications, and concept papers focused on the multidisciplinary profile of coumarins, highlighting natural sources, most recent synthetic pathways, along with the main biological applications and theoretical studies, were the main focus of this book. The huge and growing range of applications of coumarins described in this book is a demonstration of the potential of this family of compounds in Organic Chemistry, Medicinal Chemistry, and different sciences related to the study of natural products. This book includes 23 articles: 17 original papers and six review papers.
Download or read book Anticancer Agents written by Qiao-Hong Chen and published by MDPI. This book was released on 2021-03-02 with total page 606 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.
Download or read book Advances in Malaria Research written by Deepak Gaur and published by John Wiley & Sons. This book was released on 2016-12-27 with total page 611 pages. Available in PDF, EPUB and Kindle. Book excerpt: Thoroughly reviews our current understanding of malarial biology Explores the subject with insights from post-genomic technologies Looks broadly at the disease, vectors of infection, and treatment and prevention strategies A timely publication with chapters written by global researchers leaders
Download or read book Chemical Epigenetics written by Antonello Mai and published by Springer Nature. This book was released on 2020-03-31 with total page 569 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.
Download or read book Diversity Oriented Synthesis written by Andrea Trabocchi and published by John Wiley & Sons. This book was released on 2013-06-17 with total page 550 pages. Available in PDF, EPUB and Kindle. Book excerpt: Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis by describing chemical libraries Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications. Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications.
Download or read book Carbohydrate Mimics written by Yves Chapleur and published by Wiley-VCH. This book was released on 1998-09-10 with total page 638 pages. Available in PDF, EPUB and Kindle. Book excerpt: Carbohydrate Mimics Concepts and Methods Edited by Yves Chapleur Apart from the various functions of carbohydrates in natural processes they are important building blocks for drugs, especially antibiotics. In addition, carbohydrates are considered as important structures in the immunological recognition process of the antigen-antibody reaction. The modification of the structure and thereby the chemistry of substrates is a common procedure in nature. This naturally occurring process is reflected in the concept of molecular mimicry, which has become a useful approach in drug discovery. The search for carbohydrate analogues that exhibit better binding activity, biological activity, and stability began with the synthesis of azasugars. A lot of structural modifications around the anomeric center of carbohydrates has been achieved over the last decade, and these are summarized in terms of the different chemical and biological aspects of carbohydrate mimics in one part of this book. In addition to the well established fields of C-glycosides, azasugars and carbasugars the other part of the book focusses on outstanding achievements in carbohydrate mimic research. Everybody who is active in carbohydrate research or is interested in moving into this exciting field will benefit from this up-to-date source of informations. The leading experts in this field describe their scientific approaches to real interdisciplinary puzzles. This book should be an inspiration to scientists in organic, medicinal chemistry, biochemistry, and biology.
Download or read book Notes on the Synthesis of Form written by Christopher Alexander and published by Harvard University Press. This book was released on 1964 with total page 228 pages. Available in PDF, EPUB and Kindle. Book excerpt: "These notes are about the process of design: the process of inventing things which display new physical order, organization, form, in response to function." This book, opening with these words, presents an entirely new theory of the process of design. In the first part of the book, Christopher Alexander discusses the process by which a form is adapted to the context of human needs and demands that has called it into being. He shows that such an adaptive process will be successful only if it proceeds piecemeal instead of all at once. It is for this reason that forms from traditional un-self-conscious cultures, molded not by designers but by the slow pattern of changes within tradition, are so beautifully organized and adapted. When the designer, in our own self-conscious culture, is called on to create a form that is adapted to its context he is unsuccessful, because the preconceived categories out of which he builds his picture of the problem do not correspond to the inherent components of the problem, and therefore lead only to the arbitrariness, willfulness, and lack of understanding which plague the design of modern buildings and modern cities. In the second part, Mr. Alexander presents a method by which the designer may bring his full creative imagination into play, and yet avoid the traps of irrelevant preconception. He shows that, whenever a problem is stated, it is possible to ignore existing concepts and to create new concepts, out of the structure of the problem itself, which do correspond correctly to what he calls the subsystems of the adaptive process. By treating each of these subsystems as a separate subproblem, the designer can translate the new concepts into form. The form, because of the process, will be well-adapted to its context, non-arbitrary, and correct. The mathematics underlying this method, based mainly on set theory, is fully developed in a long appendix. Another appendix demonstrates the application of the method to the design of an Indian village.
Download or read book Cumulated Index Medicus written by and published by . This book was released on 1999 with total page 1846 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Antimalarial Natural Products written by A. Douglas Kinghorn and published by Springer Nature. This book was released on 2022-01-02 with total page 116 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume begins with a short history of malaria and follows with a summary of its biology. It then traces the fascinating history of the discovery of quinine for malaria treatment, and then describes quinine’s biosynthesis, its mechanism of action, and its clinical use, concluding with a discussion of synthetic antimalarial agents based on quinine’s structure. It also covers the discovery of artemisinin and its development as the source of the most effective current antimalarial drug, including summaries of its synthesis and biosynthesis, its mechanism of action, and its clinical use and resistance. A short discussion of other clinically used antimalarial natural products leads to a detailed treatment of additional natural products with significant antiplasmodial activity, classified by compound type. Although the search for new antimalarial natural products from Nature’s combinatorial library is challenging, it is very likely to yield new antimalarial drugs. This book thus ends by identifying ten natural products with development potential as clinical antimalarial agents.
Download or read book Bioisosteres in Medicinal Chemistry written by Nathan Brown and published by John Wiley & Sons. This book was released on 2012-06-18 with total page 249 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization. The third part covers the four key methodologies for bioisostere identification and replacement: physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures. In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed. With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section.
Download or read book Methylxanthines written by Bertil B. Fredholm and published by Springer Science & Business Media. This book was released on 2010-09-22 with total page 566 pages. Available in PDF, EPUB and Kindle. Book excerpt: In the present volume of the Handbook of Experimental Pharmacology well known experts describe the actions of different xanthines with a focus on caffeine and theophylline. A special chapter is devoted to theobromine, an active component of chocolate, the actions of which are less well characterized. This book also presents the pharmacology of one xanthine derivative, propentofylline, as an example of a xanthine that has gone through extensive development for a novel therapeutic area.
Download or read book How Learning Works written by Susan A. Ambrose and published by John Wiley & Sons. This book was released on 2010-04-16 with total page 336 pages. Available in PDF, EPUB and Kindle. Book excerpt: Praise for How Learning Works "How Learning Works is the perfect title for this excellent book. Drawing upon new research in psychology, education, and cognitive science, the authors have demystified a complex topic into clear explanations of seven powerful learning principles. Full of great ideas and practical suggestions, all based on solid research evidence, this book is essential reading for instructors at all levels who wish to improve their students' learning." —Barbara Gross Davis, assistant vice chancellor for educational development, University of California, Berkeley, and author, Tools for Teaching "This book is a must-read for every instructor, new or experienced. Although I have been teaching for almost thirty years, as I read this book I found myself resonating with many of its ideas, and I discovered new ways of thinking about teaching." —Eugenia T. Paulus, professor of chemistry, North Hennepin Community College, and 2008 U.S. Community Colleges Professor of the Year from The Carnegie Foundation for the Advancement of Teaching and the Council for Advancement and Support of Education "Thank you Carnegie Mellon for making accessible what has previously been inaccessible to those of us who are not learning scientists. Your focus on the essence of learning combined with concrete examples of the daily challenges of teaching and clear tactical strategies for faculty to consider is a welcome work. I will recommend this book to all my colleagues." —Catherine M. Casserly, senior partner, The Carnegie Foundation for the Advancement of Teaching "As you read about each of the seven basic learning principles in this book, you will find advice that is grounded in learning theory, based on research evidence, relevant to college teaching, and easy to understand. The authors have extensive knowledge and experience in applying the science of learning to college teaching, and they graciously share it with you in this organized and readable book." —From the Foreword by Richard E. Mayer, professor of psychology, University of California, Santa Barbara; coauthor, e-Learning and the Science of Instruction; and author, Multimedia Learning
